Abstract:
A novel compound is provided to show excellent activity on PDE-4 enzymes and high selectivity on other PDE enzymes, thereby being used as a therapeutic agent of inflammation related diseases, arthritis, atopic dermatitis, leukemia, various cancers and degenerative brain diseases with little side effects. A 1-[1-(3,4-dialkoxyphenyl)-alkyl]-1H-pyrazole compound is represented by a formula(1) and is prepared by reacting a halo-benzyl compound represented by a formula(2) with a pyrazole compound represented by a formula(3). In the formula(1), each R1 and R2 is independently H, linear or branched saturated or unsaturated C1-7 alkyl which may be substituted or unsubstituted by halogen, C3-7 cycloalkyl, (C3-7)cycloalkyl(C1-7)alkyl, aryl or heteroaryl, ar(C1-5)alkyl, or ar(C1-5)alkoxy, or the R1 and R2 may be linked to each other by C1-3 alkylene; each R3, R4 and R5 is independently H, phenyl, pyridinyl, N-oxypyridinyl, linear or branched saturated and unsaturated C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, halogen, cyano, nitro, amino, mono- or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl, C3-7 cycloalkylamino, 3 to 7-membered saturated or unsaturated hetero-ring including O, N or S, guanidinyl, ureido, benzyl, benzyloxy, formyl, C1-7 alkanoyl, C1-7 alkoxy, (C1-7)alkoxy(C1-7)alkyl, hydroxy(C1-7)alkyl, carboxyl, or (C1-7)alkoxycarbonyl; R6 is linear or branched saturated and unsaturated C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, phenyl, phenoxy, benzyl, benzyloxy, C1-7 alkoxy, or (C1-7)alkoxy(C1-7)alkyl. A pharmaceutical composition for treating or preventing diseases related to airway inflammation, arthritis, atopic dermatitis, leukemia, cancer or degenerative brain diseases comprises the 1-[1-(3,4-dialkoxyphenyl)-alkyl]-1H-pyrazole derivative as an effective ingredient.
Abstract:
A pharmaceutical composition for treating or preventing arthritis, atopic dermatitis, tumor and degenerative brain diseases comprising 7-(3,4-Dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidine compounds is provided to inhibit activity of PDE-4(phosphodiesterase-4) and reduce side effects such as vomiting by reducing HARBS(high-affinity rolipram binding sites) affinity. The pharmaceutical composition for treating or preventing arthritis, atopic dermatitis, tumor and degenerative brain diseases comprises 7-(3,4-Dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidine compounds represented by the formula(1), wherein R1 and R2 are independently hydrogen atom, linear or branched saturated or unsaturated (C1-C7)alkyl, linear or branched saturated or unsaturated (C1-C7)alkyl containing halogen atom, (C3-C7)cycloalkyl, 3-membered to 7-membered heterocycloalkyl containing oxygen, nitrogen or sulfur in a hetero aromatic ring, (C4-C10)cycloalkyl(C1-C7)alkyl, 3-membered to 7-membered heterocycloalkyl(C1-C7)alkyl containing oxygen, nitrogen or sulfur in a hetero ring, phenyl, benzyl or allyl group; R3 is hydrogen atom, halogen atom, formyl, linear or branched and saturated or unsaturated (C1-C7)alkyl, (C1-C7)alkylketone, (C1-C7)alkoxy, (C1-C7)alkoxy (C1-C7)alkyl, hydroxy(C1-C7)alkyl group, carboxylic acid, carboxyl(C1-C7)alkylester, carboxyl(C1-C7)alkylamide, amino, or mono or di(C1-C7)alkylaminocarbonyl; and R4 is hydrogen atom, formyl, linear or branched saturated or unsaturated (C1-C7)alkyl, (C3-C7)cycloalkyl, (C1-C7)alkoxy, (C1-C7)alkoxy (C1-C7)alkyl, hydroxy(C1-C7)alkyl ketone, (C1-C10)alkylcarboxylic acid, carboxyl(C1-C10)alkylester, carboxyl(C1-C10)alkylamide, amino, mono or di(C1-C7)alkylamino, mono or di(C1-C7)alkylaminocarbonyl, (C3-C7)cycloalkylamine, morpholine, morpholine oxide, piperidine, piperazine, piperazine oxide or aryl group.
Abstract:
본 발명은 하기의 화학식 1로 표시되는 신규한 4-(3,4-디알콕시페닐)-2-아미노티아졸 화합물 또는 그의 약제학적으로 허용 가능한 염, 이의 제조 방법 및 이를 유효성분으로 함유하는 것을 특징으로 하는 천식 및 만성폐쇄성 폐질환(Chronic Obstructive Pulmonary Disease)을 포함한 염증관련 질환의 치료 및 알쯔하이머를 포함한 중추신경계통 질환의 치료, 예방을 위한 약제학적 조성물에 관한 것이다. [화학식 1]
Abstract:
PURPOSE: Provided are 9-(5-isoxazolemethoxyphenyl)imino-8-thia-1,6-diazabicyclo(4.3.0)nonan-7-one derivatives which have herbicidal activity and a herbicidal composition containing the same as active ingredient. The derivatives have high stability to rice and excellent herbicidal effect. CONSTITUTION: 9-(5-isoxazolemethoxyphenyl)imino-8-thia-1,6-diazabicyclo(4.3.0)nonan-7-one derivative is represented by the formula(1), wherein R is C1-C5 alkyl group, phenyl group or substituted phenyl group in which the substituted phenyl group has a substituent selected from C1-C3 alkoxy group, halogen atom, cyano group and carboxylic acid ester group. The herbicidal composition is characterized by containing the 9-(5-isoxazolemethoxyphenyl)imino-8-thia-1,6-diazabicyclo(4.3.0)nonan-7-one derivative as active ingredient.
Abstract:
PURPOSE: Herbicidal2-(5-oxiranylmethoxyphenyl)-4,5,6,7-tetrahydro-2H-indazole derivatives are provided, which compounds have improved herbicidal effects and selectivity, so that the compounds can selectively kill weeds. CONSTITUTION: The herbicidal2-(5-oxiranylmethoxyphenyl)- 4,5,6,7-tetrahydro-2H-indazole derivatives represented by formula (1) are provided, wherein R1, R2 and R3 are independently hydrogen, C1-C5 alkyl, phenyl or substituted phenyl with 1 to 3 of halogen atoms. The method for preparing the herbicidal2-(5-oxiranylmethoxyphenyl)- 4,5,6,7-tetrahydro-2H-indazole derivatives of formula (1) comprises the steps of: reacting a compound of formula (2) with allyl halide in the presence of base to prepare a compound of formula (3); and introducing epoxy group into a double bond of the compound of formula (3), wherein X is halogen.
Abstract:
PURPOSE: Provided are derivatives of 9-(5-isoxazolinemethoxyphenyl)imino-8-thia-1.6-diazabicylco£4.3.0|nonane-7-one, represented by the formula(1) and herbicides containing them as active ingredients and having excellent herbicidal activity and selectivity when applied to a rice paddy. CONSTITUTION: Derivatives are represented by the formula(1), wherein R is C1-C6 alkyl, phenyl or substituted phenyl, wherein substituents are 1-3 of halogen atom, C1-C3 alkyl, C1-C3 alkoxy, C1-C3 haloalkyl, cyano, nitro, carboxyl and esters of carboxy acid.
Abstract:
PURPOSE: A process for preparing 3-chloro-2- (4-chloro-2-fluoro-5-hydroxyphenyl)- 4,5,6,7-tetrahydro-2H-indazole is provided, thereby improving its preparation yield and converting by-products of the preparation into starting material. CONSTITUTION: A process for preparing 3-chloro-2- (4-chloro-2-fluoro-5-hydroxyphenyl)- 4,5,6,7-tetrahydro-2H-indazole of the formula 1 comprises the steps of: reacting 2- (2-fluoro-4-chloro-5-hydroxyphenyl)- 2,3a,4,5,6,7- hexahydroindazole-3-one of the formula 2 with phosgene; concentrating the phosgene reaction mixture under reduced pressure; dissolving the concentrate in an organic solvent; adding ammonia water or hydroxide solution to the organic solvent and filtering solids; and distilling the filtrated solution, wherein the organic solvent is ethylacetate; the addition of ammonia water or hydroxide solution is carried out at room temperature; the solids are mainly constituted of a compound of the formula 2, and the by-products of the reaction include a dimer represented by the formula 3a, 3b or 3c.
Abstract:
PURPOSE: Provided is 5-benzyloxymethyl-1,2-isoxazoline derivative which has an excellent herbicidal activity. Also, provided are its manufacturing method and herbicides containing the derivative as an active ingredient. CONSTITUTION: 5-benzyloxymethyl-1,2-isoxazoline derivative is represented by the formula(I), wherein X1, X2 and X3 individually represent hydrogen, methyl group, ethyl group, halogen group, methoxy group or nitro group (provided that it is an exception that X1, X2 and X3 are decimals all together); Y1, Y2 and Y3 are individually hydrogen or fluorine.